Linagliptin (8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione) acts as a dipeptidyl peptidase IV (DPP IV) inhibitor and is currently used in the treatment of type 2 diabetes mellitus.
WO2004/018468 discloses linagliptin, salts thereof, a process for the preparation of linagliptin and its salts, and the use of linagliptin, and its salts for the treatment of certain diseases.
WO2007/128721 describes crystalline forms A, B, C, D, and E of linagliptin and processes for preparing the crystalline forms. It also discloses that linagliptin prepared according to WO2004/018468 is in the form of a mixture of crystalline form A and crystalline form B.
WO2007/128724 discloses a pharmaceutical composition comprising a DPP IV inhibitor compound with an amino group, such as linagliptin or a salt thereof, a first diluent, a second diluent, a binder, a disintegrant and a lubricant.
WO2014/026939 discloses a pharmaceutical composition comprising linagliptin or salts thereof with mannitol, copovidone, and magnesium stearate, a process for the preparation of the pharmaceutical composition, and a container comprising the pharmaceutical composition.
However, there is the need to provide a pharmaceutical composition which can be obtained by a more efficient manufacturing process without the use of solvents and with a low number of process steps. In particular, a low number of excipients should be used to reduce complexity of the process, specifically to reduce the number of manual interventions (adding excipients, mixing steps), to reduce the number of analytical processes to be applied (release analytics for each excipient prior to use) and to reduce overall production costs. The pharmaceutical composition obtained by said more efficient manufacturing process nevertheless needs to have suitable properties allowing handling on an industrial scale in high speed manufacturing equipment and at the same time a fast dissolution in the gastrointestinal tract after administration together with a suitable content uniformity of the active ingredient and a sufficient storage stability. The content uniformity is of special importance because linagliptin is present in a pharmaceutical composition in a low amount of about 0.5 to 5% by weight.